Clotrimazole, an antifungal drug possessing diverse actions, increases the vulnerability to cadmium in lymphocytes dissociated from rat thymus

Oyama, Tomohiro M.; Oyama, Toshihisa B.; Oyama, Kenichi; Matsui, Hiroko; Horimoto, Kanna; Nishimura, Yumiko; Oyama, Yasuo

doi:10.1016/j.tox.2006.09.007

Cited by 6 publications

(4 citation statements)

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“…), and it has been reported to exert neuroprotective effects and to modify the cytotoxicity of some metal cations (Oyama et al . ). There is much interest in the therapeutic application of clotrimazole in sickle cell disease, because its metabolite, ICA 17043, is believed to exert a beneficial effect on erythrocyte dehydration by blocking the Gardos calcium channel (Brugnara et al .…”

Section: Brief Summary Of Antimicrobial Activitymentioning

confidence: 97%

Clotrimazole as a pharmaceutical: past, present and future.

2014

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Summary Clotrimazole is a broad‐spectrum antimycotic drug mainly used for the treatment of Candida albicans and other fungal infections. A synthetic, azole antimycotic, clotrimazole is widely used as a topical treatment for tinea pedis (athlete's foot), as well as vulvovaginal and oropharyngeal candidiasis. It displays fungistatic antimycotic activity by targeting the biosynthesis of ergosterol, thereby inhibiting fungal growth. As well as its antimycotic activity, clotrimazole has become a drug of interest against several other diseases such as sickle cell disease, malaria and some cancers. It has also been combined with other molecules, such as the metals, to produce clotrimazole complexes that show improved pharmacological efficacy. Moreover, several new, modified‐release pharmaceutical formulations are also undergoing development. Clotrimazole is a very well‐tolerated product with few side effects, although there is some drug resistance appearing among immunocompromised patients. Here, we review the pharmaceutical chemistry, application and pharmacology of clotrimazole and discuss future prospects for its further development as a chemotherapeutic agent.

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Section: Brief Summary Of Antimicrobial Activitymentioning

confidence: 97%

Clotrimazole as a pharmaceutical: past, present and future.

2014

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“…Compound (1) 95.58 (14) 89.95 (11) 115.83 (10) 114.41(9) N(3)\M,M′(1)\X,X′ (2) 95.70 (14) 91.42 (12) 113.45 (11) 117.32(8) N(1)\M,M′(1)\X,X′ (2) 93.82 (14) 91.15 (11) 114.56 (6) 108.54(9) N(5)\Cu(2)\N (7) 158.4(2) ---N(5)\Cu(2)\Cl (5) 91.42(15) ---N(7)\Cu(2)\Cl (5) 93.92(15) ---N(5)\Cu(2)\Cl (6) 92.36 (14) ---N(7)\Cu(2)\Cl (6) 94.39 (14) ---M_Cu, M′_Zn, X_Cl, X′_Br.…”

Section: Crystal Structuresmentioning

confidence: 99%

“…Thus, the use of metal complexes as chemotherapeutic agents is well established [7], particularly in the cancer field for cisplatin and related compounds [8,9]. Examples of the synergistic applications of clotri with CdCl 2 or PbCl 2 have been shown to significantly increase cell lethality of rat thymocytes [10], whereas the combination of ZnCl 2 and clotri has proved to accelerate the process of apoptosis in this type of rat cells [11]. The synthesis and characterization of new Ru II , Cu II , and Au I -clotri complexes [12,13] have also been reported.…”

Section: Introductionmentioning

confidence: 99%

Cytotoxic copper(II), cobalt(II), zinc(II), and nickel(II) coordination compounds of clotrimazole

Betanzos-Lara

Gómez-Ruíz

Barrón-Sosa

et al. 2012

Journal of Inorganic Biochemistry

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“…Its efficacy includes the treatment of human infection of pathogenic dermatophytes and yeasts. CTZ is a potent enzyme inhibitor which may cause several drug interactions [8,9]. Thus, topical administration is a suitable approach to avoid this problem.…”

Section: Introductionmentioning

confidence: 99%

Antidermatophytic Activity and Skin Retention of Clotrimazole Microemulsion and Microemulsion-Based Gel in Comparison to Conventional Cream

Kaewbanjong

Amnuaikit

Souto

et al. 2018

Skin Pharmacol Physiol

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Aim: Antifungal activity, skin permeation and skin retention of water-in-oil microemulsion (ME) and microemulsion-based gel (MBG) containing clotrimazole (CTZ) were evaluated in comparison to a conventional CTZ cream. Methods: CTZ-ME and CTZ-MBG containing 1% w/w of CTZ were produced. Antifungal activity against Trichophyton mentagrophytes was assessed by the agar diffusion method. Pig skin was used in the in vitro penetration study using modified Franz diffusion cells. Drug amounts which permeated into the receptor fluid, retained in the skin membrane and remained in the donor compartment were analyzed by a validated HPLC technique. Results: CTZ-ME and CTZ-MBG exhibited inhibition zones against T. mentagrophytes whereas the conventional cream did not reveal any inhibition zone in the assay. While no CTZ was detected in the receptor fluid up to 24 h following the in vitro penetration study from all tested formulations, the amount of CTZ retained in the skin membrane when applying CTZ-ME and CTZ-MBG was remarkably higher than that when applying the cream. Conclusion: Results revealed the capacity of ME and MBG in improving skin bioavailability of CTZ while reducing the risk of systemic side effects. Thereby, ME and MBG could increase the efficacy of CTZ for dermatophytosis treatment in comparison to conventional cream.

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Clotrimazole, an antifungal drug possessing diverse actions, increases the vulnerability to cadmium in lymphocytes dissociated from rat thymus

Cited by 6 publications

References 50 publications

Clotrimazole as a pharmaceutical: past, present and future.

Clotrimazole as a pharmaceutical: past, present and future.

Cytotoxic copper(II), cobalt(II), zinc(II), and nickel(II) coordination compounds of clotrimazole

Antidermatophytic Activity and Skin Retention of Clotrimazole Microemulsion and Microemulsion-Based Gel in Comparison to Conventional Cream

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